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马兜铃酸毒性控制研究进展

中文摘要英文摘要

马兜铃属(Aristolochia spp.)及细辛属(Asarum spp.)等马兜铃科植物作为传统中药的重要来源,其含有的萜类、生物碱等活性成分已被证实具有抗肿瘤、免疫调节及广谱抗菌等药理活性。然而,该类植物普遍存在的硝基菲羧酸类化合物--马兜铃酸(Aristolochic acids, AAs),经代谢活化后可形成DNA加合物,诱发TP53基因特征性突变及肾小管上皮细胞坏死,导致马兜铃酸肾病(AAN)及上尿路上皮癌(UTUC)。国际癌症研究机构(IARC)已将其列为Group 1人类致癌物。当前研究聚焦于建立"效-毒成分分离"技术体系,通过定向提取、生物转化及结构修饰等策略,在保留药用活性组分的同时实现马兜铃酸类成分的精准去除,这对推动含马兜铃科药材的临床安全应用具有重大意义。本文综述了马兜铃酸的毒性机制、检测技术及减毒存效技术方法,力求在"传统经验用药"向"循证精准用药"转型背景下,总结现代药毒理学理论与分离工程技术,为实现中药毒性成分"可识别、可控制、可转化"的范式创新,助力构建中药安全性研究技术体系。

Plants from the Aristolochiaceae family,such as those from the genus Aristolochia spp.and Asarum spp.,are important sources of traditional Chinese medicine.The active components they contain,such as terpenoids and alkaloids,have been proven to have pharmacological activities including anti-tumor effects,immune regulation,and broad-spectrum antibacterial properties.However,these plants also contain nitrophenanthrene carboxylic acid compounds-aristolochic acids(AAs).After metabolic activation,AAs can form DNA adducts,induce characteristic mutations in the TP53 gene,and cause necrosis of renal tubular epithelial cells,leading to aristolochic acid nephropathy(AAN)and upper urinary tract urothelial carcinoma(UTUC).The International Agency for Research on Cancer(IARC)has classified them as Group 1 human carcinogens. Current research is focused on establishing a technical system for the separation of"efficacious and toxic components."Through strategies such as targeted extraction,biotransformation,and structural modification,it aims to precisely remove AA components while retaining the active medicinal fractions.This is of great significance for promoting the safe clinical application of medicinal materials from the Aristolochiaceae family. This article reviews the toxicity mechanisms,detection technologies,and detoxification methods while retaining efficacy of aristolochic acids.Under the context of transitioning from"traditional empirical medication"to"evidence-based and precise medication,"it summarizes modern pharmacotoxicological theories and separation engineering technologies.This review aims to contribute to the paradigm innovation of"identifiable,controllable,and transformable"toxic components in traditional Chinese medicine,and to assist in the construction of a technical system for the safety research of traditional Chinese medicine.

栗新尧&、叶序韬*、李昊彤*、龙林邦、李雅萱、赵青&、谢杭羽*

天津科技大学生物工程学院,天津 300457天津科技大学生物工程学院,天津 300457天津科技大学生物工程学院,天津 300457天津科技大学生物工程学院,天津 300457天津科技大学生物工程学院,天津 300457天津科技大学生物工程学院,天津 300457;齐齐哈尔龙江阜丰生物科技有限公司,黑龙江省齐齐哈尔 161031天津科技大学生物工程学院,天津 300457

医药卫生理论医学研究方法中医学基础医学药学

马兜铃酸毒性机制检测技术减毒存效

ristolochic acidoxicity mechanismetection technologytoxicity reduction while retaining efficacy

栗新尧&,叶序韬*,李昊彤*,龙林邦,李雅萱,赵青&,谢杭羽*.马兜铃酸毒性控制研究进展[EB/OL].(2025-04-22)[2025-04-26].http://www.paper.edu.cn/releasepaper/content/202504-186.点此复制

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